WO2013035081A3 - Formulation optimale pour la libération d'un principe actif dans le gros intestin - Google Patents

Formulation optimale pour la libération d'un principe actif dans le gros intestin Download PDF

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Publication number
WO2013035081A3
WO2013035081A3 PCT/IB2012/054655 IB2012054655W WO2013035081A3 WO 2013035081 A3 WO2013035081 A3 WO 2013035081A3 IB 2012054655 W IB2012054655 W IB 2012054655W WO 2013035081 A3 WO2013035081 A3 WO 2013035081A3
Authority
WO
WIPO (PCT)
Prior art keywords
formulation
controlled release
mammal
digestive tract
several substances
Prior art date
Application number
PCT/IB2012/054655
Other languages
German (de)
English (en)
Other versions
WO2013035081A2 (fr
Inventor
Roland Saur-Brosch
Original Assignee
JÄNISCH, Melisa
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=47832673&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2013035081(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by JÄNISCH, Melisa filed Critical JÄNISCH, Melisa
Priority to EP12829553.2A priority Critical patent/EP2753310B1/fr
Priority to US14/343,393 priority patent/US10799460B2/en
Priority to AU2012305915A priority patent/AU2012305915B2/en
Priority to CA2885680A priority patent/CA2885680C/fr
Publication of WO2013035081A2 publication Critical patent/WO2013035081A2/fr
Publication of WO2013035081A3 publication Critical patent/WO2013035081A3/fr
Priority to US14/207,638 priority patent/US10653631B2/en
Priority to IN2618CHN2014 priority patent/IN2014CN02618A/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4891—Coated capsules; Multilayered drug free capsule shells
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K33/24—Heavy metals; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/167—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
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    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
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    • A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
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    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
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    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
    • A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
    • A61K9/5078—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings with drug-free core
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/167—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
    • A61K9/1676—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface having a drug-free core with discrete complete coating layer containing drug
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Mycology (AREA)
  • Microbiology (AREA)
  • Inorganic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Molecular Biology (AREA)
  • Nutrition Science (AREA)
  • Transplantation (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne une formulation pour la libération contrôlée de principes actifs après le passage de la valvule iléo-caecale, comprenant un ou plusieurs principes actifs ou bien un ou plusieurs noyaux (W) contenant un principe actif, enrobés d'une ou de plusieurs enveloppes (C) qui sont solubles ou perméables au-delà d'une valeur pH individuelle déterminée et en-deça d'une autre valeur pH individuelle déterminée, étant elles-mêmes entourées d'une enveloppe (E) qui est soluble ou perméable au-delà d'encore une autre valeur pH déterminée.
PCT/IB2012/054655 2011-09-07 2012-09-07 Formulation optimale pour la libération d'un principe actif dans le gros intestin WO2013035081A2 (fr)

Priority Applications (6)

Application Number Priority Date Filing Date Title
EP12829553.2A EP2753310B1 (fr) 2011-09-07 2012-09-07 Formulation optimale pour la libération d'un principe actif dans le gros intestin
US14/343,393 US10799460B2 (en) 2011-09-07 2012-09-07 Formulation for the controlled release of one or several substances in the digestive tract of a mammal
AU2012305915A AU2012305915B2 (en) 2011-09-07 2012-09-07 Formulation for the controlled release of one or several substances in the digestive tract of a mammal
CA2885680A CA2885680C (fr) 2011-09-07 2012-09-07 Formulation optimale pour la liberation d'un principe actif dans le gros intestin.
US14/207,638 US10653631B2 (en) 2011-09-07 2014-03-13 Optimal colon targeting technology
IN2618CHN2014 IN2014CN02618A (fr) 2011-09-07 2014-04-07

Applications Claiming Priority (18)

Application Number Priority Date Filing Date Title
DE102011112501 2011-09-07
DE102011112501.2 2011-09-07
DE102011112761 2011-09-11
DE102011112761.9 2011-09-11
DE102011056646.5 2011-12-19
DE102011056646 2011-12-19
EP12163060 2012-04-03
EP12163060.2 2012-04-03
EP12164414 2012-04-17
EP12164414.0 2012-04-17
EP12166248.0 2012-04-30
EP12166248 2012-04-30
EP12168985.5 2012-05-22
EP12168985 2012-05-22
EP12170634 2012-06-01
EP12170634.5 2012-06-01
EP12180485.0 2012-08-14
EP12180485 2012-08-14

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
US201414343393A Continuation-In-Part 2011-09-07 2014-06-16

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US14/207,638 Continuation-In-Part US10653631B2 (en) 2011-09-07 2014-03-13 Optimal colon targeting technology

Publications (2)

Publication Number Publication Date
WO2013035081A2 WO2013035081A2 (fr) 2013-03-14
WO2013035081A3 true WO2013035081A3 (fr) 2013-05-02

Family

ID=47832673

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2012/054655 WO2013035081A2 (fr) 2011-09-07 2012-09-07 Formulation optimale pour la libération d'un principe actif dans le gros intestin

Country Status (7)

Country Link
US (1) US10799460B2 (fr)
EP (1) EP2753310B1 (fr)
JP (2) JP2014529630A (fr)
AU (1) AU2012305915B2 (fr)
CA (1) CA2885680C (fr)
IN (1) IN2014CN02618A (fr)
WO (1) WO2013035081A2 (fr)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10653631B2 (en) 2011-09-07 2020-05-19 Roland SAUR-BROSCH Optimal colon targeting technology
RS56839B1 (sr) 2012-04-30 2018-04-30 Tillotts Pharma Ag Formulacija leka sa odloženim otpuštanjem
EP4385503A3 (fr) * 2013-03-15 2024-08-28 Capsugel Belgium NV Revêtement enterique pour des gélules souples
US10799515B2 (en) 2013-10-29 2020-10-13 Tillotts Pharma Ag Delayed release drug formulation
EP3773513A4 (fr) * 2018-04-12 2022-05-18 BPSI Holdings LLC Revêtements acidifiants et substrats résistant à la désagrégation revêtus de ceux-ci
AU2021396978A1 (en) 2020-12-08 2023-02-23 Ruminant Biotech Corp Limited Improvements to devices and methods for delivery of substances to animals
US20240226045A9 (en) * 2022-10-25 2024-07-11 Balchem Corporation Rumen-protected compositions and methods of making the same

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US10799460B2 (en) 2020-10-13
CA2885680C (fr) 2022-10-04
WO2013035081A2 (fr) 2013-03-14
JP2018065846A (ja) 2018-04-26
JP6659922B2 (ja) 2020-03-04
US20140302134A1 (en) 2014-10-09
IN2014CN02618A (fr) 2015-06-26
JP2014529630A (ja) 2014-11-13
CA2885680A1 (fr) 2013-03-14
AU2012305915B2 (en) 2017-09-07

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